XL-3158
Based on 1 Customer Validation
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.55%
- No. CAS: 3117797-77-7
- Fòrmula: C30H17F7N6O2S2
- Peso molecular:690.61
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
XL-3158 (Compound XL-3158) (20 μM, 4 h) blocks cGAS intracellular condensation with DNA by inhibiting cGAS phase separation in L929 cells[1].
XL-3158 (10-40 μM, 4 h) specifically inhibits downstream signaling activation of the cGAS-STING pathway in THP-1 Dual cells[1].
XL-3158 (10 μM, 4 h) selectively inhibits the DNA-triggered cGAS-dependent interferon pathway in THP-1 Dual cells[1].
XL-3158 (0-20 μM, 24 h) has CC50 values of 77.55 μM against THP-1 cells and 56.79 μM against RAW-ISG cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 Dual cells
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Concentration:10 μM, 20 μM, 40μM
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Incubation Time:4 h
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Result:Inhibited HT-DNA-induced TBK-1 and IRF3 phosphorylation in a dose-dependent manner.
Had no inhibitory effect on pathways activated by Poly (I:C) or cGAMP.
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Cell Line:THP-1 Dual cells
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Concentration:10 μM, 20 μM, 40μM
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Incubation Time:4 h
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Result:Significantly reduced HT-DNA-induced IFN-β1 mRNA expression.
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Cell Line:L929 cells
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Concentration:20 μM
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Incubation Time:4 h
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Result:Significantly reduced the number of co-localized condensates of cGAS and Cy5-DNA.
Confirmed that the condensates had liquid-like properties (LLPS) and inhibited their formation.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cerulean (HY-A0190) (50 µg/kg, i.p, injections once every hour for 7 times) induced acute pancreatitis model in C57BL/6J nude female mice (6-8 weeks)[1].
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Dosage:25mg/kg
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Administration:Intragastric gavage (i.g.), administration at 0 hour and 6 h after the first Cerulein injection.
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Result:Significantly reduced pancreatic pathological damage and the pancreas/body weight ratio, indicating that pancreatic edema was relieved.
Significantly reduced serum amylase and serum lipase activities.
Significantly reduced serum inflammatory factor levels.
Chemical Information
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No. CAS 3117797-77-7
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Appearance Solid
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Peso molecular 690.61
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Fòrmula C30H17F7N6O2S2
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Color Off-white to light yellow
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SMILES
CC1=NN(C(O)=C1C(C2=C(N(N=C2C)C3=NC4=C(S3)C=C(C=C4F)F)O)C5=CC=C(C(F)(F)F)C=C5)C6=NC7=C(S6)C=C(C=C7F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (72.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.4480 mL | 7.2400 mL | 14.4800 mL | 36.1999 mL |
| 5 mM | 0.2896 mL | 1.4480 mL | 2.8960 mL | 7.2400 mL | |
| 10 mM | 0.1448 mL | 0.7240 mL | 1.4480 mL | 3.6200 mL | |
| 15 mM | 0.0965 mL | 0.4827 mL | 0.9653 mL | 2.4133 mL | |
| 20 mM | 0.0724 mL | 0.3620 mL | 0.7240 mL | 1.8100 mL | |
| 25 mM | 0.0579 mL | 0.2896 mL | 0.5792 mL | 1.4480 mL | |
| 30 mM | 0.0483 mL | 0.2413 mL | 0.4827 mL | 1.2067 mL | |
| 40 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9050 mL | |
| 50 mM | 0.0290 mL | 0.1448 mL | 0.2896 mL | 0.7240 mL | |
| 60 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
XL-3158 Related Classifications
HY-174802 Related Classifications
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